1-benzhydryl-3-(biphenyl-4-yloxy)azetidine | 227304-95-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 1-benzhydryl-3-(biphenyl-4-yloxy)azetidine
• 英文别名: 1-Benzhydryl-3-(4-phenylphenoxy)azetidine
• CAS: 227304-95-2
• 化学式: C₂₈H₂₅NO
• 分子量: 391.513
• InChiKey: AXVCRZHDBMSXJO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.6
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-benzhydryl-3-(biphenyl-4-yloxy)azetidine 在 1-氯乙基氯甲酸酯 、 甲醇 作用下， 以 二氯甲烷 为溶剂， 以72%的产率得到3-(biphenyl-4-yloxy)azetidine hydrochloride
  参考文献：
  名称：

  [EN] AZETIDINE DERIVATIVES
  [FR] DÉRIVÉS D'AZÉTIDINE

  摘要：

  式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗状况具有益处，如焦虑、抑郁、疼痛、炎症、进食、睡眠、神经退行性和运动障碍：式（I）其中Ar1是可选择取代的苯基或可选择取代的具有5或6个环原子的单环杂芳基；Ar2是可选择取代的苯基，可选择取代的具有5或6个环原子的单环杂芳基或在每个融合环中具有5或6个环原子的可选择取代的融合双环杂芳基；Ar3是从可选择取代的苯基和可选择取代的具有5或6个环原子的单环杂芳基基团组成的羰基基团。

  公开号：

  WO2009109743A1
• 作为产物：
  描述：

  N-二苯甲基氮杂环丁烷-3-醇 、 对羟基联苯 在 三苯基膦 、 偶氮二甲酸二异丙酯 作用下， 以 乙腈 为溶剂， 反应 0.33h， 以79%的产率得到1-benzhydryl-3-(biphenyl-4-yloxy)azetidine
  参考文献：
  名称：

  [EN] AZETIDINE DERIVATIVES
  [FR] DÉRIVÉS D'AZÉTIDINE

  摘要：

  式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗状况具有益处，如焦虑、抑郁、疼痛、炎症、进食、睡眠、神经退行性和运动障碍：式（I）其中Ar1是可选择取代的苯基或可选择取代的具有5或6个环原子的单环杂芳基；Ar2是可选择取代的苯基，可选择取代的具有5或6个环原子的单环杂芳基或在每个融合环中具有5或6个环原子的可选择取代的融合双环杂芳基；Ar3是从可选择取代的苯基和可选择取代的具有5或6个环原子的单环杂芳基基团组成的羰基基团。

  公开号：

  WO2009109743A1

文献信息

• Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
  申请人：Warner-Lambert Company

  公开号：US06495568B1

  公开（公告）日：2002-12-17

  Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin diseases.

  化合物的式子(I)：或其药学上或兽医学上可接受的盐，或这两个实体的药学上或兽医学上可接受的溶剂化物，其中断线代表可选键；A为C或CH；B为CH2、O或不存在；R1和R2各自独立地选自氢、C1至C6烷基，可选地被C1至C4烷氧基或苯基取代，以及C1至C6烯基；或与它们所连接的碳原子一起形成C3至C6环烷基，该环烷基可选地包括从O、SO、SO2和NR6中选择的杂原子键合或可选地与苯融合；R3为氢、卤素、R7或OR7；R4为氢、C1至C4烷基、C1至C4烷氧基、三氟甲基或卤素；R6为氢或C1至C4烷基；R7为可选取代的单环或双环环系统；m为1或2；n为0、1或2；但当A为C时，B不为O；这些MMP抑制剂在治疗组织溃疡、伤口修复和皮肤疾病等方面非常有用。
• Azetidine derivatives as FAAH inhibitors
  申请人：Roughley Stephen

  公开号：US08450346B2

  公开（公告）日：2013-05-28

  Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

  公式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗条件的治疗非常有用，如焦虑、抑郁、疼痛、炎症、进食、睡眠、神经退行性和运动障碍等： 公式（I）中，Ar1是可选择的取代苯基或可选择的取代的含有5或6个环原子的单环杂芳基；Ar2是可选择的取代苯基、可选择的取代含有5或6个环原子的单环杂芳基或可选择的取代融合的双环杂芳基，在每个融合环中有5或6个环原子；Ar3是从可选择的取代苯撑基和可选择的取代含有5或6个环原子的单环杂芳撑基的群中选择的二价基团。
• Azetidine Derivatives
  申请人：Roughley Stephen

  公开号：US20120028953A1

  公开（公告）日：2012-02-02

  Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Formula (I) Wherein Ar 1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar 2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar 3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

  公式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗条件具有治疗作用，例如焦虑、抑郁、疼痛、炎症、饮食、睡眠、神经退行性和运动障碍：公式（I）中，Ar1是可选取取代苯基或可选取取代的5或6个环原子的单环杂芳基；Ar2是可选取取代苯基、可选取取代的5或6个环原子的单环杂芳基或在每个融合环中具有5或6个环原子的可选取取代的融合双环杂芳基；而Ar3是从可选取取代的苯基和可选取取代的5或6个环原子的单环杂芳基组成的二价基团中选择的。
• Azetidine derivatives
  申请人：Vernalis (R&D) Ltd.

  公开号：US09006269B2

  公开（公告）日：2015-04-14

  Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

  式（I）的化合物是脂肪酸酰胺水解酶（FAAH）的抑制剂，对于需要抑制FAAH活性的疾病或医疗状况具有治疗作用，例如焦虑、抑郁、疼痛、炎症、进食、睡眠、神经退行性和运动障碍： 其中Ar1是可以选择性取代的苯基或具有5或6个环原子的可以选择性取代的单环杂芳基；Ar2是可以选择性取代的苯基，具有5或6个环原子的可以选择性取代的单环杂芳基或在每个融合环中具有5或6个环原子的可以选择性取代的融合双环杂芳基；Ar3是从包括可以选择性取代的苯撑基和具有5或6个环原子的可以选择性取代的单环杂芳撑基的基团中选择的二价基团。
• US6387931
  申请人：——

  公开号：——

  公开（公告）日：——